Preparation of Prolonged-Release Spherical Micro-Matrix of Ibuprofen with Acrylic Polymer by the Emulsion-Solvent Diffusion Method for Improving Bioavailability

Abstract

Prolonged-release spherical micro-matrices of ibuprofen with acrylic polymer (Eudragit^[○!R] RS) were prepared using a novel emulsion-solvent diffusion metho. It was found by examining cross sections of the spherical matrix before and after dissolution tests with a scanning electron microscope and a porosimeter that the resultant micro-matrix had a sponge-like internal structure. The spherical matrices were successfully recovered with a relatively high concentration of the drug in ethanol (0.4-0.6g/ml) and over a wide range of temperatures (5-35°C). The size of the spherical matrix could be easily controlled by varying the agitation speed of the system and the concentration of emulsifier added to the aqueous medium. The drug release rate from the spherical matrix decreased with increasing concentration of polymer formulated due to the reduced diffusion path and increased tortuosity in the matrix. Spherical matrices with ibuprofen : Eudragit^[○!R] RS=3 : 1 improved the bioavailability of the drug and prolonged the drug action in beagle dogs.